A PHASE 1, OPEN-LABEL, NON-RANDOMIZED, 2-PERIOD, FIXED SEQUENCE STUDY TO INVESTIGATE THE ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF 14C-PF-06651600 AND TO ASSESS THE ABSOLUTE BIOAVAILABILITY AND FRACTION ABSORBED OF PF-06651600 IN HEALTHY MALE PARTICIPANTS USING A 14C-MICROTRACER APPROACH
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Pfizer
- 入组人数
- 6
- 试验地点
- 2
- 主要终点
- Mass Balance: Cumulative recovery (%) of radioactivity in urine
研究概览
简要总结
This study will investigate the absorption, distribution, metabolism and excretion (ADME) of 14C PF-06651600 and characterize plasma, fecal and urinary radioactivity and identify any metabolites, if possible, of 14C PF-06651600 in humans.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Sequential
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Male participants who are healthy as determined by medical evaluation including a detailed medical history, full physical examination, including blood pressure (BP) and pulse rate (PR) measurement, 12 lead ECG, and clinical laboratory tests.
- •Body mass index (BMI) of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
排除标准
- •Known immunodeficiency disorder, including positive serology for human immunodeficiency virus (HIV) at screening, or a first degree relative with a hereditary immunodeficiency.
- •Infection with hepatitis B or hepatitis C viruses.
- •Participants with selected acute or chronic infections or infection history.
- •Participants have a known present or a history of malignancy other than a successfully treated or excised non metastatic basal cell or squamous cell cancer of the skin.
- •History of alcohol abuse or binge drinking and/or any other illicit drug use or dependence within 6 months of Screening.
- •Use of tobacco/nicotine containing products within 3 months prior to dosing or positive urine cotinine test.
研究组 & 干预措施
Period A
Single oral dose of 200 mg 14C labeled PF-06651600 containing approximately 300 nCi 14C (ie, radiolabeled PF 06651600).
干预措施: 14C-PF-06651600 (Drug)
Period B
Single oral dose of 200 milligrams (mg) unlabeled PF-06651600 followed at time of peak plasma concentration (Tmax) by an Intravenous (IV) dose of 60 micrograms.14C -PF-06651600 containing approximately 300 nCi 14C (ie, radiolabeled PF-06651600).
干预措施: 14C-PF-06651600 IV (Drug)
Period B
Single oral dose of 200 milligrams (mg) unlabeled PF-06651600 followed at time of peak plasma concentration (Tmax) by an Intravenous (IV) dose of 60 micrograms.14C -PF-06651600 containing approximately 300 nCi 14C (ie, radiolabeled PF-06651600).
干预措施: PF-06651600 (Drug)
结局指标
主要结局
Mass Balance: Cumulative recovery (%) of radioactivity in urine
时间窗: from time zero to the time of last measurable concentration following oral administration of 14C PF-06651600 microtracer dose up to day 24
Cumulative recovery (%) of radioactivity in urine.
Mass Balance: Cumulative recovery (%) of radioactivity in feces
时间窗: from time zero to the time of last measurable concentration following oral administration of 14C PF-06651600 microtracer dose up to day 24
Cumulative recovery (%) of radioactivity in feces
次要结局
- Number of Participants With Clinically Significant Change From Baseline in Vital Signs(Baseline (Day 0) up to Day 24)
- Number of Participants With Clinically Significant Change From Baseline in Laboratory Abnormalities(Baseline (Day 0) up to Day 24)
- Amount (% of the administered dose) of major metabolites of PF-06651600 in urine(Hour 0 up to 312 hours post-dose.)
- AUClast(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- AUCinf(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- Tmax(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- CL (IV)(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- Vz/F(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- Total 14C_Urine_PO(Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose)
- Amount (% of the administered dose) of major metabolites of PF-06651600 in plasma(Hour 0 up to 312 hours post-dose.)
- Amount (% of the administered dose) of major metabolites of PF-06651600 in feces(Hour 0 up to 312 hours post-dose.)
- t1/2(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- CL/F (oral)(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- Cmax(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- Vss(Pre-dose, 0.25. 0.5, 1, 1.5, 2, 3.5, 4.5, 6.5, 8.5, 12.5, 24, 48, 72, 96 hours post-dose)
- Total 14C_Urine_IV(Pre-dose, Day1, day 2, day 3, day 4, day 5, day 6 and day 7 post-dose)
- AE(Baseline (Day 0) up to 90 days after last dose of study medication)
- Number of participants with clinically significant changes to the physical examination(Baseline (Day 0) up to Day 24)